Fluoroquinolones: General Pharmacology

Fluoroquinolones (1/5): general pharmacology
Fluoroquinolones (2/5): ciprofloxacin
Fluoroquinolones (3/5): levofloxacin
Fluoroquinolones (4/5): ofloxacin
Fluoroquinolones (5/5): norfloxacin

Review literature: (Mombelli et al, 1999) (Naber et al, 1999) (Simon and Stille, 1997).

Substances of the Fluoroquinolone Family:

Fluoroquinolones, which are commonly used in urology are ciprofloxacin, levofloxacin, norfloxacin and ofloxacin.

Mechanism of Action of Fluoroquinolones:

Fluoroquinolones interfere with the bacterial DNA synthesis via inhibition of the DNA gyrase or topoisomerase II. Fluoroquinolone antibiotics are bactericidal.

Indications for Fluoroquinolones:

Fluoroquinolones are active against a variety of bacteria:

Gram-negative pathogens including Pseudomonas, Mycoplasma, Chlamydia,..
Gram-positive pathogens, but not Pneumococci or Enterococci
Some anaerobic bacteria

Indications for fluoroquinolones are urinary tract infection (increasing resistance), prostatitis, acute pyelonephritis, epididymitis, perioperative antibiotic prophylaxis for transurethral surgery, bronchitis, pneumonia, sinusitis, gastrointestinal infections, soft tissue infections.

Pharmacokinetics of Fluoroquinolones:

Fluoroquinolones have a good bioavailability after oral administration.
Good tissue penetration
Most common renal elimination

Side Effects of Fluoroquinolones:

Gastrointestinal side effects: Nausea, vomiting, diarrhea, pseudomembranous colitis
Neurotoxicity with headache, dizziness, psychosis and seizures.
Allergy
Photosensitization
Orthopedic side effects: cartilage damage, tendon damage with spontaneous tendon rupture.

Contraindications to Fluoroquinolones:

Pregnancy and lactation
Epilepsy
Stroke
Severe renal insufficiency
QT-prolongation
Caution in children: cartilage damage

Urologic Surgery

Index

Ciprofloxacin

Index: 1–9 A B C D E F G H I J K L M N O P Q R S T U V W X Y Z

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References

Auquer u.a. 2002 AUQUER, F. ; CORDON, F. ; GORINA, E. ; CABALLERO, J. C. ; ADALID, C. ; BATLLE, J.:: Single-dose ciprofloxacin versus 3 days of norfloxacin in uncomplicated urinary tract infections in women.
In: Clin Microbiol Infect
8 (2002), Nr. 1, S. 50–4
Henry u.a. 2002 HENRY, Jr. ; BETTIS, R. B. ; RIFFER, E. ; HAVERSTOCK, D. C. ; KOWALSKY, S. F. ; MANNING, K. ; HAMED, K. A. ; CHURCH, D. A.:: Comparison of once-daily extended-release ciprofloxacin and conventional twice-daily ciprofloxacin for the treatment of uncomplicated urinary tract infection in women.
In: Clin Ther
24 (2002), Nr. 12, S. 2088–104
Krcmery und Naber 1999 KRCMERY, S. ; NABER, K. G.:: Ciprofloxacin once versus twice daily in the treatment of complicated urinary tract infections. German Ciprofloxacin UTI Study Group.
In: Int J Antimicrob Agents
11 (1999), Nr. 2, S. 133–8
Martin u.a. 1998 MARTIN, S. J. ; MEYER, J. M. ; CHUCK, S. K. ; JUNG, R. ; MESSICK, C. R. ; PENDLAND, S. L.:: Levofloxacin and sparfloxacin: new quinolone antibiotics.
In: Ann Pharmacother
32 (1998), Nr. 3, S. 320–36
Mombelli u.a. 1999 MOMBELLI, G. ; PEZZOLI, R. ; PINOJA-LUTZ, G. ; MONOTTI, R. ; MARONE, C. ; FRANCIOLLI, M.:: Oral vs. intravenous ciprofloxacin in the initial empirical management of severe pyelonephritis or complicated urinary tract infections: a prospective randomized clinical trial.
In: Arch Intern Med
159 (1999), Nr. 1, S. 53–8
Naber u.a. 1999 NABER, K. G. ; THEURETZBACHER, U. ; MONEVA-KOUCHEVA, G. ; STASS, H.:: Urinary excretion and bactericidal activity of intravenous ciprofloxacin compared with oral ciprofloxacin.
In: Eur J Clin Microbiol Infect Dis
18 (1999), Nr. 11, S. 783–9
Raz u.a. 2000 RAZ, R. ; NABER, K. G. ; RAIZENBERG, C. ; ROHANA, Y. ; UNAMBA-OPARAH, I. ; KORFMAN, G. ; YANIV, I.:: Ciprofloxacin 250 mg twice daily versus ofloxacin 200 mg twice daily in the treatment of complicated urinary tract infections in women.
In: Eur J Clin Microbiol Infect Dis
19 (2000), Nr. 5, S. 327–31
Reid u.a. 2000 REID, G. ; POTTER, P. ; DELANEY, G. ; HSIEH, J. ; NICOSIA, S. ; HAYES, K.:: Ofloxacin for the treatment of urinary tract infections and biofilms in spinal cord injury.
In: Int J Antimicrob Agents
13 (2000), Nr. 4, S. 305–7
Simon und Stille 1997 SIMON, C. ; STILLE, W.:: Antibiotika-Therapie in Klinik und Praxis.
9. Auflage.
Stuttgart New York : Schattauer, 1997
Talan u.a. 2004 TALAN, D. A. ; KLIMBERG, I. W. ; NICOLLE, L. E. ; SONG, J. ; KOWALSKY, S. F. ; CHURCH, D. A.:: Once daily, extended release ciprofloxacin for complicated urinary tract infections and acute uncomplicated pyelonephritis.
In: J Urol
171 (2004), Nr. 2 Pt 1, S. 734–9

Deutsche Version: Fluoroquinolone (Gyrasehemmer)

Last update

Dr. med. Dirk Manski
man...@urologielehrbuch.de